阿苯达唑.|54965-21-8|(阿苯达唑; SKF-62979)-陌孚医药/Medlife

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阿苯达唑. (Synonyms: 阿苯达唑; SKF-62979)

目录号: PC12864 纯度: ≥98%

CAS No. :54965-21-8

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PC12864-100mg	100mg	¥490.00	请登录
PC12864-1g	1g	¥780.00	请登录
PC12864-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥539.00	请登录

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中文名称

阿苯达唑.

中文别名

丙硫咪唑;阿苯达唑;阿苯唑;扑尔虫;肠虫清;抗蠕敏;丙硫多菌灵悬浮剂;[5-(丙硫基)-1H-苯并咪唑-2-基]氨基甲酸甲酯;[5-(丙基硫代)-1H-苯并咪唑-2-基]氨基甲酸甲酯;5-丙硫基-苯并咪唑-2-氨基甲酸甲酯;丙硫苯咪唑;阿苯哒唑;阿苯哒唑标准品;阿苯哒唑杂质;阿苯达唑 EP标准品;阿苯达唑 USP标准品;阿苯达唑标准品;阿苯达唑；丙硫达唑;阿苯达唑药典标准;氨基甲酸甲酯;丙硫咪唑杂质对照品;丙硫咪唑原药;[5-(丙基硫代)苯并咪唑-2-基]氨基甲酸甲酯;5-(丙硫基)-2-苯并咪唑氨基甲酸甲酯;甲基[5-(丙基硫代)苯并咪唑-2-基]氨基甲酸酯;抗寄生虫;阿苯达唑杂质

英文名称

Albendazole; SKF-62979

英文别名

albendazole;Albendazole suspension;[5-(PROPYLTHIO)-1H-BENZIMIDAZOL-2-YL]CARBAMIC ACID, METHYL ESTER;[5-(PROPYLTHIO)BENZIMIDAZOL-2-YL]CARBAMIC ACID METHYL ESTER;(5-PROPYLSULFANYL-1H-BENZOIMIDAZOL-2-YL)-CARBAMIC ACID METHYL ESTER;ALBAZINE;ALBEN;ALBENZA;AKOS NCG1-0064;5-propylthio-2-carbomethoxyaminobenzimidazole;Atasol;Bilutac;Bruzol;methyl [5-(propylsulfanyl)-1H-1,3-benzimidazol-2-yl]carbamate;Methyl [5-(Propylthio)BenziMidazol-2-yl]CarbaMate;methyl 5-(propylthio)benzimidazol-2-ylcarbamate;methyl N-[5-(propylthio)-1H-benzimidazol-2-yl]carbamate;methyl-5-propylthio-2-benzimidazole carbamate;Monil;ZEBEN;ZENTEL;Methyl 5-propylthio-2-benzimidazolecarbamate;Eskazole;Valbazen;Proftril;Albendazolum;Albendazol;Zental;SK&F 62979;SKF 62979;Methyl 5-(propylthio)-2-benzimidazolecarbamate;Albendazolum [INN-Latin];Albendazol [INN-Spanish];5-(Propylthio)-2-carbomethoxyaminobenzimidazole;methyl N-[6-(propylsulfanyl)-1H-1,3-benzodiazol-2-yl]carbamate;(5-(Propylthio)-1H-benzimidazol-2-yl)carbamic acid methyl ester;O-Methyl N-(5-(propylthi

Cas No.

54965-21-8

分子式

C₁₂H₁₅N₃O₂S

分子量

265.33

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Albendazole (SKF-62979) is an orally active and broad-spectrum parasiticide with high effectiveness and low host toxicity, is used for the research of gastrointestinal parasites in humans and animals. Albendazole induces apoptosis and autophagy in cancer cells. Albendazole also inhibits tubulin polymerization and HIF-1α, VEGF expression, has antioxidant activity, and inhibits the glycolytic process in cancer cells.

性状

Solid

IC50 & Target[1][2]

parasites, tubulin.
HIF-1α, VEGF.

体外研究(In Vitro)

Albendazole (100, 500, 1000 nM; 1, 3, or 5 days) inhibits cell proliferation in a dose-dependent manner.
Albendazole (100, 250, 500, 1000 nM; 3 days) arrests SKHEP-1 cells at both G0–G1 (250, 500 nM) and G2-M (1000 nM) phases of the cycle.
Albendazole (5 μM; 24, 36 h) mainly induces early apoptosis in HCT-15 cells and late apoptosis in HCT-1 16, HT29, SW480 cells accompanied with cleavage of PARP and caspase-3 in a time-dependent manner.
Albendazole (5 μM; 24, 36 h) induces autophagy via increasing autophagy-related protein (such as LC3, Atg7, p-beclin-1, and beclin-1) expression level in HCT-15, HCT-1 16, HT29, and SW480 cells.
Albendazole (500 nM, 24 h) inhibits hypoxia-induced HIF-1α expression and VEGF expression in A549 cells.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	SKHEP-1 cells
Concentration:	100, 500, 1000 nM
Incubation Time:	1, 3, or 5 days
Result:	Inhibited cell proliferation in a dose-dependent manner.

Cell Cycle Analysis

Cell Line:	SKHEP-1 HCC cells
Concentration:	100, 250, 500, 1000 nM
Incubation Time:	3 days
Result:	Showed dose-dependent effect on the cell cycle kinetics.

Apoptosis Analysis

Cell Line:	HCT-15, HCT-1 16, HT29, SW480 cells
Concentration:	5 μM
Incubation Time:	24, 36 h
Result:	Promoted apoptosis in colon cancer cells.

Cell Autophagy Assay

Cell Line:	HCT-15, HCT-1 16, HT29, SW480 cells
Concentration:	5 μM
Incubation Time:	24, 36 h
Result:	Induced autophagy in colon cancer cells.

Western Blot Analysis

Cell Line:	HCT-15, HCT-1 16, HT29, SW480 cells
Concentration:	5 μM
Incubation Time:	12, 24, 36 h
Result:	Induced apoptosis-related protein (PARP, caspase-3) and autophagy-related protein (such as LC3, Atg7, p-beclin-1, and beclin-1) expression level in a time-dependent manner. Increased phosphorylation of different MAPKs (AMPK, ERK, JNK, p38) and ULK1 protein in a time dependent manner, and up-regulated the activation of different MAPKs. Caused the activation of both MAPK and AMPK pathways.

Western Blot Analysis

Cell Line:	A549 cells
Concentration:	500 nM
Incubation Time:	24 h
Result:	Inhibited hypoxia-induced HIF-1α expression and VEGF expression in A549 cells.

体内研究(In Vivo)

Albendazole (10 mg/kg; i.g.; once a day for 30 days) reduces Echinococcus granulosus cyst weights in mice.
Albendazole (300 mg/kg; p.o.; per day in two divided dose for 20 days) profoundly suppresses tumor growth in vivo.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female BALB/c mice (10-week-age; Echinococcus granulosus infection model).
Dosage:	10 mg/kg
Administration:	Oral gavage; once a day for 30 days.
Result:	Reduced Echinococcus granulosus cyst weights.

Animal Model:	Male BALB/c Nu/Nu mice (6 to 10-week-old; inoculated subcutaneously with SKHEP-1).
Dosage:	50, 150, 300 mg/kg
Administration:	Oral administration; per day in two divided dose for 20 days.
Result:	Profoundly suppressed tumor growth in vivo.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Pourgholami MH, et al. 体外研究 and in vivo suppression of growth of hepatocellular carcinoma cells by albendazole. Cancer Lett. 2001 Apr 10;165(1):43-9. [Information]

[2]. Jung YY, et al. Regulation of apoptosis and autophagy by albendazole in human colon adenocarcinoma cells. Biochimie. 2022 Jul;198:155-166. [Information]

[3]. Zhou F, et al. Albendazole inhibits HIF-1α-dependent glycolysis and VEGF expression in non-small cell lung cancer cells. Mol Cell Biochem. 2017 Apr;428(1-2):171-178. [Information]

[4]. Vural G, et al. Efficacy of novel albendazole salt formulations against secondary cystic echinococcosis in experimentally infected mice. Parasitology. 2020 Nov;147(13):1425-1432. [Information]

[5]. Li L, et al. Determination of albendazole and metabolites in silkworm Bombyx mori hemolymph by ultrafast liquid chromatography tandem triple quadrupole mass spectrometry. PLoS One. 2014 Sep 25;9(9):e105637. [Information]

溶解度数据

体外研究:

DMSO : 20 mg/mL (75.38 mM; Need ultrasonic)

H₂O : 0.67 mg/mL (2.53 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.7689 mL	18.8445 mL	37.6889 mL
5 mM	0.7538 mL	3.7689 mL	7.5378 mL
10 mM	0.3769 mL	1.8844 mL	3.7689 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2 mg/mL (7.54 mM); Suspended solution; Need ultrasonic

此方案可获得 2 mg/mL (7.54 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2 mg/mL (7.54 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (7.54 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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